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In vitro anti-Leishmania activity and molecular docking of spiro-acridine compounds as potential multitarget agents against Leishmania infantum.

Authors :
Almeida FS
Sousa GLS
Rocha JC
Ribeiro FF
de Oliveira MR
de Lima Grisi TCS
Araújo DAM
de C Nobre MS
Castro RN
Amaral IPG
Keesen TSL
de Moura RO
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2021 Oct 01; Vol. 49, pp. 128289. Date of Electronic Publication: 2021 Jul 24.
Publication Year :
2021

Abstract

Leishmaniasis is an infectious disease with several limitations regarding treatment schemes. This work reports the anti-Leishmania activity of spiroacridine compounds against the promastigote (IC <subscript>50</subscript>  = 1.1 to 6.0 µg / mL) and amastigote forms of the best compounds (EC <subscript>50</subscript>  = 4.9 and 0.9 µg / mL) inLeishmania (L.) infantumand proposes an in-silico study with possible selective therapeutic targets for L. infantum. The substituted dimethyl-amine compound (AMTAC 11) showed the best leishmanicidal activity in vitro, and was found to interact with TryRandLdTopoI. comparisons with standard inhibitors were performed, and its main interactions were elucidated. Based on the biological assessment and the structure-activity relationship study, the spiroacridine compounds appear to be promisinganti-leishmaniachemotherapeutic agents to be explored.<br /> (Copyright © 2021 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
49
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
34311084
Full Text :
https://doi.org/10.1016/j.bmcl.2021.128289